| 货号 | 18287-1mg |
| 描述 | Mocetinostat is an orally available inhibitor of histone deacetylases (HDACs) that selectively targets HDAC1 and 2 (IC50s = 0.15 and 0.29 µM, respectively), less potently inhibits HDAC3 and 11 (IC50s = 1.66 and 0.59 µM, respectively) and has negligible actions against HDAC4-8.1,2 It induces hyperacetylation of histones, causes cell cycle blockade, and induces apoptosis in cancer cells in vitro.1,3 Mocetinostat also has antitumor activity in vivo, blocking the growth of human tumor xenografts in mice.1 It also significantly reduces cardiac fibrosis following ischemic heart failure in mice.4 |
| 别名 | MGCD0103; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Fournel, M.,Bonfils, C.,Hou, Y., et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Molecular Cancer Therapeutics 7(4), 759-768 (2008). 2.Marson, C.M.,Matthews, C.J.,Atkinson, S.J., et al. Potent and selective inhibitors of histone deacetylase-3 containing chiral oxazoline capping groups and a N-(2-aminophenyl)-benzamide binding unit. Journal of Medicinal Chemistry 58, 6803-6818 (2015). 3.Bonfils, C.,Kalita, A.,Dubay, M., et al. Evaluation of the pharmacodynamic effects of MGCD0103 from preclinical models to human using a novel HDAC enzyme assay. Clinical Cancer Research 14(11), 3441-3449 (2008). 4.Nural-Guvener, H.,Zakharova, L.,Feehery, L., et al. Anti-fibrotic effects of class I HDAC inhibitor, mocetinostat is associated with IL-6/Stat3 signaling in ischemic heart failure. International Journal of Molecular Sciences 16, 11482-11499 (2015). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 396.4 |
| 分子式 | C23H20N6O |
| CAS号 | 726169-73-9 |
| 稳定性 | ≥ 2 years |
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